Page last updated: 2024-11-12

a-438079

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cross-References

ID SourceID
PubMed CID11673921
CHEMBL ID377219
SCHEMBL ID5815398
MeSH IDM0514679

Synonyms (22)

Synonym
3-[[5-(2,3-dichlorophenyl)tetrazol-1-yl]methyl]pyridine
CHEMBL377219 ,
a-438079
a438079 ,
AKOS016035814
bdbm50410955
a 438079
HY-15488
CS-1293
NCGC00347906-01
3-((5-(2,3-dichlorophenyl)-1h-tetrazol-1-yl)methyl)pyridine
3-{[5-(2,3-dichlorophenyl)-1h-1,2,3,4-tetrazol-1-yl]methyl}pyridine
gtpl4118
MMPAULQSJLVKHP-UHFFFAOYSA-N
3-{[5-(2,3-dichlorophenyl)-1h-tetraazol-1-yl]methyl}pyridine
SCHEMBL5815398
3-[[5-(2,3-dichlorophenyl)-1h-tetrazol-1-yl]methyl]pyridine
NCGC00347906-04
3-[5-(2,3-dichloro-phenyl)-tetrazol-1-ylmethyl]-pyridine
Q27074072
HMS3748O07
MS-24422

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (11)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency4.25340.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency21.31740.01238.964839.8107AID1645842
Interferon betaHomo sapiens (human)Potency21.31740.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency21.31740.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency21.31740.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency21.31740.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Transient receptor potential cation channel subfamily A member 1Homo sapiens (human)IC50 (µMol)0.05900.05102.47257.5000AID1913032; AID1913329
P2X purinoceptor 7Rattus norvegicus (Norway rat)IC50 (µMol)0.43210.00470.43211.9000AID1831763; AID266264; AID321350; AID423046; AID597637
P2X purinoceptor 7Rattus norvegicus (Norway rat)Ki0.20000.00200.20250.5100AID1831767
P2X purinoceptor 7Homo sapiens (human)IC50 (µMol)0.48300.00080.24525.0000AID1358119; AID1831762; AID266262; AID321349; AID423041; AID597636
P2X purinoceptor 7Homo sapiens (human)Ki0.06800.00310.03150.0680AID1831766
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki0.50550.00000.490110.0000AID1915176
P2X purinoceptor 7Mus musculus (house mouse)IC50 (µMol)2.90000.00070.98542.9000AID1831764
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (135)

Processvia Protein(s)Taxonomy
monoatomic ion transportTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
intracellular calcium ion homeostasisTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
cell surface receptor signaling pathwayTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
response to coldTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
response to xenobiotic stimulusTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
response to organic substanceTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
response to organic cyclic compoundTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
sensory perception of painTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
calcium-mediated signalingTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
response to painTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
thermoceptionTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
detection of mechanical stimulus involved in sensory perception of painTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
detection of chemical stimulus involved in sensory perception of painTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
protein homotetramerizationTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
cellular response to hydrogen peroxideTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
calcium ion transmembrane transportTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
cellular response to organic substanceTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
MAPK cascadeP2X purinoceptor 7Homo sapiens (human)
cell morphogenesisP2X purinoceptor 7Homo sapiens (human)
phagolysosome assemblyP2X purinoceptor 7Homo sapiens (human)
T cell mediated cytotoxicityP2X purinoceptor 7Homo sapiens (human)
positive regulation of T cell mediated cytotoxicityP2X purinoceptor 7Homo sapiens (human)
positive regulation of protein phosphorylationP2X purinoceptor 7Homo sapiens (human)
regulation of sodium ion transportP2X purinoceptor 7Homo sapiens (human)
response to ischemiaP2X purinoceptor 7Homo sapiens (human)
membrane protein ectodomain proteolysisP2X purinoceptor 7Homo sapiens (human)
phospholipid transfer to membraneP2X purinoceptor 7Homo sapiens (human)
vesicle budding from membraneP2X purinoceptor 7Homo sapiens (human)
inflammatory responseP2X purinoceptor 7Homo sapiens (human)
mitochondrion organizationP2X purinoceptor 7Homo sapiens (human)
cell surface receptor signaling pathwayP2X purinoceptor 7Homo sapiens (human)
protein secretionP2X purinoceptor 7Homo sapiens (human)
response to xenobiotic stimulusP2X purinoceptor 7Homo sapiens (human)
response to mechanical stimulusP2X purinoceptor 7Homo sapiens (human)
response to zinc ionP2X purinoceptor 7Homo sapiens (human)
positive regulation of calcium ion transport into cytosolP2X purinoceptor 7Homo sapiens (human)
positive regulation of gene expressionP2X purinoceptor 7Homo sapiens (human)
glutamate secretionP2X purinoceptor 7Homo sapiens (human)
positive regulation of glutamate secretionP2X purinoceptor 7Homo sapiens (human)
gamma-aminobutyric acid secretionP2X purinoceptor 7Homo sapiens (human)
positive regulation of gamma-aminobutyric acid secretionP2X purinoceptor 7Homo sapiens (human)
synaptic vesicle exocytosisP2X purinoceptor 7Homo sapiens (human)
protein processingP2X purinoceptor 7Homo sapiens (human)
plasma membrane phospholipid scramblingP2X purinoceptor 7Homo sapiens (human)
sensory perception of painP2X purinoceptor 7Homo sapiens (human)
calcium-mediated signalingP2X purinoceptor 7Homo sapiens (human)
protein catabolic processP2X purinoceptor 7Homo sapiens (human)
positive regulation of bone mineralizationP2X purinoceptor 7Homo sapiens (human)
bleb assemblyP2X purinoceptor 7Homo sapiens (human)
positive regulation of prostaglandin secretionP2X purinoceptor 7Homo sapiens (human)
prostaglandin secretionP2X purinoceptor 7Homo sapiens (human)
response to lipopolysaccharideP2X purinoceptor 7Homo sapiens (human)
positive regulation of interleukin-1 alpha productionP2X purinoceptor 7Homo sapiens (human)
positive regulation of interleukin-1 beta productionP2X purinoceptor 7Homo sapiens (human)
positive regulation of interleukin-6 productionP2X purinoceptor 7Homo sapiens (human)
collagen metabolic processP2X purinoceptor 7Homo sapiens (human)
response to ATPP2X purinoceptor 7Homo sapiens (human)
response to fluid shear stressP2X purinoceptor 7Homo sapiens (human)
positive regulation of monoatomic ion transmembrane transportP2X purinoceptor 7Homo sapiens (human)
purinergic nucleotide receptor signaling pathwayP2X purinoceptor 7Homo sapiens (human)
T cell proliferationP2X purinoceptor 7Homo sapiens (human)
T cell homeostasisP2X purinoceptor 7Homo sapiens (human)
NAD transportP2X purinoceptor 7Homo sapiens (human)
negative regulation of MAPK cascadeP2X purinoceptor 7Homo sapiens (human)
positive regulation of MAPK cascadeP2X purinoceptor 7Homo sapiens (human)
negative regulation of bone resorptionP2X purinoceptor 7Homo sapiens (human)
negative regulation of cell volumeP2X purinoceptor 7Homo sapiens (human)
positive regulation of glycolytic processP2X purinoceptor 7Homo sapiens (human)
ceramide biosynthetic processP2X purinoceptor 7Homo sapiens (human)
pore complex assemblyP2X purinoceptor 7Homo sapiens (human)
skeletal system morphogenesisP2X purinoceptor 7Homo sapiens (human)
homeostasis of number of cells within a tissueP2X purinoceptor 7Homo sapiens (human)
positive regulation of protein secretionP2X purinoceptor 7Homo sapiens (human)
defense response to Gram-positive bacteriumP2X purinoceptor 7Homo sapiens (human)
release of sequestered calcium ion into cytosolP2X purinoceptor 7Homo sapiens (human)
positive regulation of cytoskeleton organizationP2X purinoceptor 7Homo sapiens (human)
response to calcium ionP2X purinoceptor 7Homo sapiens (human)
response to electrical stimulusP2X purinoceptor 7Homo sapiens (human)
mitochondrial depolarizationP2X purinoceptor 7Homo sapiens (human)
membrane depolarizationP2X purinoceptor 7Homo sapiens (human)
positive regulation of mitochondrial depolarizationP2X purinoceptor 7Homo sapiens (human)
excitatory postsynaptic potentialP2X purinoceptor 7Homo sapiens (human)
positive regulation of macrophage cytokine productionP2X purinoceptor 7Homo sapiens (human)
T cell apoptotic processP2X purinoceptor 7Homo sapiens (human)
positive regulation of T cell apoptotic processP2X purinoceptor 7Homo sapiens (human)
cellular response to ATPP2X purinoceptor 7Homo sapiens (human)
cellular response to dsRNAP2X purinoceptor 7Homo sapiens (human)
reactive oxygen species metabolic processP2X purinoceptor 7Homo sapiens (human)
apoptotic signaling pathwayP2X purinoceptor 7Homo sapiens (human)
extrinsic apoptotic signaling pathwayP2X purinoceptor 7Homo sapiens (human)
positive regulation of bleb assemblyP2X purinoceptor 7Homo sapiens (human)
calcium ion transmembrane transportP2X purinoceptor 7Homo sapiens (human)
lipid transportSigma non-opioid intracellular receptor 1Homo sapiens (human)
nervous system developmentSigma non-opioid intracellular receptor 1Homo sapiens (human)
G protein-coupled opioid receptor signaling pathwaySigma non-opioid intracellular receptor 1Homo sapiens (human)
regulation of neuron apoptotic processSigma non-opioid intracellular receptor 1Homo sapiens (human)
protein homotrimerizationSigma non-opioid intracellular receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (27)

Processvia Protein(s)Taxonomy
calcium channel activityTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
channel activityTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
intracellularly gated calcium channel activityTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
identical protein bindingTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
temperature-gated cation channel activityTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
lipopolysaccharide bindingP2X purinoceptor 7Homo sapiens (human)
purinergic nucleotide receptor activityP2X purinoceptor 7Homo sapiens (human)
extracellularly ATP-gated monoatomic cation channel activityP2X purinoceptor 7Homo sapiens (human)
signaling receptor bindingP2X purinoceptor 7Homo sapiens (human)
protein bindingP2X purinoceptor 7Homo sapiens (human)
ATP bindingP2X purinoceptor 7Homo sapiens (human)
identical protein bindingP2X purinoceptor 7Homo sapiens (human)
G protein-coupled opioid receptor activitySigma non-opioid intracellular receptor 1Homo sapiens (human)
protein bindingSigma non-opioid intracellular receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (40)

Processvia Protein(s)Taxonomy
plasma membraneTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
stereocilium bundleTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneP2X purinoceptor 7Rattus norvegicus (Norway rat)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmP2X purinoceptor 7Homo sapiens (human)
mitochondrionP2X purinoceptor 7Homo sapiens (human)
plasma membraneP2X purinoceptor 7Homo sapiens (human)
cell-cell junctionP2X purinoceptor 7Homo sapiens (human)
external side of plasma membraneP2X purinoceptor 7Homo sapiens (human)
membraneP2X purinoceptor 7Homo sapiens (human)
neuromuscular junctionP2X purinoceptor 7Homo sapiens (human)
blebP2X purinoceptor 7Homo sapiens (human)
neuronal cell bodyP2X purinoceptor 7Homo sapiens (human)
presynapseP2X purinoceptor 7Homo sapiens (human)
postsynapseP2X purinoceptor 7Homo sapiens (human)
plasma membraneP2X purinoceptor 7Homo sapiens (human)
nuclear envelopeSigma non-opioid intracellular receptor 1Homo sapiens (human)
nuclear inner membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
nuclear outer membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulumSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulum membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
lipid dropletSigma non-opioid intracellular receptor 1Homo sapiens (human)
cytosolSigma non-opioid intracellular receptor 1Homo sapiens (human)
postsynaptic densitySigma non-opioid intracellular receptor 1Homo sapiens (human)
membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
growth coneSigma non-opioid intracellular receptor 1Homo sapiens (human)
cytoplasmic vesicleSigma non-opioid intracellular receptor 1Homo sapiens (human)
anchoring junctionSigma non-opioid intracellular receptor 1Homo sapiens (human)
postsynaptic density membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulumSigma non-opioid intracellular receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (60)

Assay IDTitleYearJournalArticle
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1831767Displacement of [3H]-A-804598 from rat P2X7 receptor expressed in HEK293 cell membrane by in vitro binding assay2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139.
AID423041Antagonist activity at P2X7 receptor in human THP1 cells assessed as inhibition of BzATP-induced ethidium uptake2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Antagonists of the P2X(7) receptor. From lead identification to drug development.
AID760096Antagonist activity at P2X7 in Sprague-Dawley rat synaptosome assessed as inhibition of BzATP-induced [3H]D-aspartate efflux preincubated at 10 uM for 8 mins by liquid scintillation counting in absence of extracellular Ca2+2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
Flow Synthesis and Biological Studies of an Analgesic Adamantane Derivative That Inhibits P2X7-Evoked Glutamate Release.
AID266268Oral bioavailability in rat at 10 umol/kg, ip2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists.
AID266265Inhibition of ILbeta production in human THP1 cells2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists.
AID266262Antagonist activity at human P2X7 receptor expressed in human 1321N1 cells assessed as inhibition of calcium flux by FLIPR2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists.
AID266266Reversal of mechanical allodynia in L5/L6 spinal nerve tight ligation model of neuropathic pain in ip dosed rat2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists.
AID1831766Displacement of [3H]-A-804598 from human P2X7 receptor expressed in HEK293 cell membrane by in vitro binding assay2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139.
AID1831763Antagonist activity at rat P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium-flux measured after 60 mins by FLIPR analysis2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139.
AID266264Antagonist activity at rat P2X7 receptor expressed in human 1321N1 cells assessed as inhibition of calcium flux by FLIPR2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists.
AID597637Antagonist activity at rat recombinant P2X7 receptor expressed in HEK293 cells assessed as inhibition of benzoylbenzoic ATP-induced calcium production by FLIPR assay2011Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11
Synthesis and in vitro activity of N-benzyl-1-(2,3-dichlorophenyl)-1H-tetrazol-5-amine P2X(7) antagonists.
AID266263Ability to block pore formation in human THP1 cells assessed as inhibition of YO-PRO-1 diiodide dye uptake2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists.
AID760099Antagonist activity at P2X7 in Sprague-Dawley rat synaptosome assessed as inhibition of BzATP-induced [3H]D-aspartate efflux preincubated at 10 uM for 8 mins by liquid scintillation counting2013ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8
Flow Synthesis and Biological Studies of an Analgesic Adamantane Derivative That Inhibits P2X7-Evoked Glutamate Release.
AID597636Antagonist activity at human recombinant P2X7 receptor expressed in HEK293 cells assessed as inhibition of benzoylbenzoic ATP-induced calcium production by FLIPR assay2011Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11
Synthesis and in vitro activity of N-benzyl-1-(2,3-dichlorophenyl)-1H-tetrazol-5-amine P2X(7) antagonists.
AID423163Bioavailability in ip dosed rat2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Antagonists of the P2X(7) receptor. From lead identification to drug development.
AID266267Reversal of mechanical allodynia in L5/L6 spinal nerve tight ligation model of neuropathic pain in ip dosed rat relative to control2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists.
AID321349Antagonist activity at human recombinant P2X7 receptor assessed as inhibition of BzATP-induced calcium flux by FLIPR assay2008Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
Synthesis and in vitro activity of 1-(2,3-dichlorophenyl)-N-(pyridin-3-ylmethyl)-1H-1,2,4-triazol-5-amine and 4-(2,3-dichlorophenyl)-N-(pyridin-3-ylmethyl)-4H-1,2,4-triazol-3-amine P2X7 antagonists.
AID423164Half life in ip dosed rat2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Antagonists of the P2X(7) receptor. From lead identification to drug development.
AID1694069Antagonist activity at P2X7R in mouse N2a cells assessed as reduction in ATP-induced calcium influx at 5 uM incubated for 1 hr by Fura-2AM dye based spectrofluorometry relative to control2021Bioorganic & medicinal chemistry, 02-01, Volume: 31Synthetic 1,4-Naphthoquinones inhibit P2X7 receptors in murine neuroblastoma cells.
AID423046Activity at rat P2X7 receptor expressed in HEK cells assessed as effect on BzATP-induced ethidium uptake2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Antagonists of the P2X(7) receptor. From lead identification to drug development.
AID321350Antagonist activity at rat recombinant P2X7 receptor assessed as inhibition of BzATP-induced calcium flux by FLIPR assay2008Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
Synthesis and in vitro activity of 1-(2,3-dichlorophenyl)-N-(pyridin-3-ylmethyl)-1H-1,2,4-triazol-5-amine and 4-(2,3-dichlorophenyl)-N-(pyridin-3-ylmethyl)-4H-1,2,4-triazol-3-amine P2X7 antagonists.
AID266270Impairment of motor function in rat by rotarod assay up to 300 umol/kg, ip2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists.
AID1358119Antagonist activity at human P2X7 receptor in expressed in HEK293 cells assessed as inhibition of BzATP-induced EtBr uptake
AID1831762Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium-flux measured after 60 mins by FLIPR analysis2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139.
AID1831764Antagonist activity at mouse P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium-flux measured after 60 mins by FLIPR analysis2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139.
AID266269Half life in rat at 10 umol/kg2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists.
AID1831769Metabolic stability in human liver microsomes assessed as intrinsic clearance at 1 uM incubated for 60 mins by LC-MS/MS analysis2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139.
AID1831770Metabolic stability in rat liver microsomes assessed as intrinsic clearance at 1 uM incubated for 60 mins by LC-MS/MS analysis2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346612Human P2X7 (P2X receptors)2007British journal of pharmacology, Jul, Volume: 151, Issue:5
Discovery of P2X7 receptor-selective antagonists offers new insights into P2X7 receptor function and indicates a role in chronic pain states.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (16)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's4 (25.00)29.6817
2010's5 (31.25)24.3611
2020's7 (43.75)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 19.60

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index19.60 (24.57)
Research Supply Index2.83 (2.92)
Research Growth Index4.80 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (19.60)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (12.50%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other14 (87.50%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]